Although numerous medications have the potential to treat central nervous system (CNS) disorders, only a small number of these drugs have actually been used successfully. It is as a result of the blood–brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSF) preventing them from exerting biological activity by allowing them to cross the brain. The current methods for enhancing penetration across these barriers for efficient CNS medication delivery are reviewed in this article. Direct systemic delivery, invasive delivery, BBB disruption, and convection enhanced delivery are a summary of these problems. Additionally, cutting-edge nanoscale drug delivery methods such polymeric nanoparticles, liposomes, nanoemulsions, dendrimers, and micelles are explored. These nanocarriers might lead to a development in the treatment of numerous CNS illnesses. To evaluate the biocompatibility and safety of these medical devices, however, further extensive research is required.